UNC-8969

UNC-8969 : Inhibitor of MERTK, AXL

Structure

SERP Rating

Probe UNC-8969 is in the process of SERP review.

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Information

MERTK
AXL

Inhibitor

100 nM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: Q12866

Target Class: Kinase

Target SubClass: Tyrosine kinase

Potency: IC50

Potency Value: 1.1 nM

Potency Assay: Biochemical assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Tyrosine-protein kinase Mer, MER, MERTK, MERTK_HUM ...

DOI Reference: 10.1021/acs.jmedchem.4c00148

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): The selectivity of UNC8969 against other members of the kinome was evaluated in a Off-chip Mobility Shift Assay using a 32-kinase panel including MERTK, AXL, and TYRO3 at 110 nM (100-fold above its MERTK IC50). Both MERTK and AXL were fully inhibited, while TYRO3 was inhibited partially (67%) at this concentration. Only one other kinase (KDR) was inhibited greater than 80% in the presence of 110 nM UNC8969 and none of the serine/threonine kinases were appreciably inhibited. In a kinase activity assay IC50 for Tyro was 66 nM and for FLT3 70 nM.

Potency assay, off target (cells): Selectivity against TYRO3 was confirmed using NanoBRET EC50 >4 uM

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